The study of LY03015 has been published in European Journal of Medicinal Chemistry, a publication of French Société de Chimie Thérapeutique. The study shows that LY03015 demonstrated a high binding affinity for VMAT2 with excellent inhibition of DA uptake, and promising drug-like properties with good liver microsome stability and robust pharmacokinetic properties in rats. Compared with the VMAT2 inhibitors currently used to treat TD or/ and HD, such as tetrabenazine, deutetrabenazine and valbenazine, LY03015 is expected to reduce risks of serious adverse reactions such as depression and suicide due to the off-target effects. Consistent with the improved pharmacokinetics, a favorable prolonged half-life may enable its once daily administration. Moreover, good brain penetration, lower distribution in thꦚe heart tissue and lower effect on hERG, may enable administration at lower dosages, with fewer side effects (e.g., QTc prolongation). The results suggest that 13e might be a promising candida𒀰te for TD and HD treatment, with better safety and efficacy profiles.
In the future, based on the further validation of its properties in clinical trials, LY03015 is expected to address the unmet treatment needs of patients using commercially available VMAT2 inhibitors in terms of activity, efficacy and safety. Publicly available data shows that three VMAT2 inhibitors approved by the U.S. Food and Drug Administration (FDA) had combined global sales of approximately US $1.659 billion in 2020, an increase of 37.9% over 2019, indicating significant market potential. The CNS therapeutic area, which LY03015 belongs to, is one of the strategic focuses for Luye Pharma. The company has developed a range of differentiated innovative drugs and innovative formulations on its innovative technology platforms including NCE/NTE platform and Novel Drug Delivery Systems platform, with breakthroughs being constantly achieved for its pipeline.In January 2021, Rykindo® (Risperidone Microspheres for Injection (Ⅱ)) for the treatment of schizophrenia was approved for launch in China. This product is also China’s first locally developed innovative microsphere formulation. In addition, the Rivastigmine Multi-Day Transdermal Patch for treating Alzheimer’s disease has also been approved for launch in several European countries. The company’s Seroquel® (Quetiapine Fumarate Tablets, immediate release, IR) and Seroquel XR® (Quetiapine Fumarate Exten💝ded-Release Tablets) for treating schizophrenia and bipolar disorder are so๊ld in 51 countries and regions worldwide.
In addition to products that have already been launched, the company also has a number of new drugs under development, and several of them are now in the late stage of clinical development or the New Drug Application (NDA) stage in China, the U.S., and other markets, covering a variety of CNS diseases such as depression and Parkinson’s disease. Together, they form a strong CNS portfolio.